TD-0212( TD0212 | TD 0212 )

Catalog No. M10302 CAS No. 1073549-10-6

TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP).

Purity : >98% (HPLC)

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Biological Information

Product Name

TD-0212
Note

Research use only, not for human use.
Brief Description

TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP).
Description

TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP); produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and -independent hypertension, does not increase TPE at antihypertensive doses in rat tracheal plasma extravasation (TPE) models.
In Vitro

TD-0212 (compound 35) provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition.
In Vivo

TD-0212 (compound 35) produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and –independent hypertension.
Synonyms

TD0212 | TD 0212
Pathway

GPCR/G Protein
Target

Angiotensin Receptor
Recptor

Angiotensin Receptor
Research Area

——
Indication

——

Chemical Information

CAS Number

1073549-10-6
Formula Weight

527.655
Molecular Formula

C28H34FN3O4S
Purity

>98% (HPLC)
Solubility

——
SMILES

CCC1=C(N(C(=N1)OCC)CC2=C(C=C(C=C2)C3=CC=CC=C3C(=O)O)F)CNC(=O)C(CC(C)C)S
Chemical Name

(S)-4'-((2-ethoxy-4-ethyl-5-((2-mercapto-4-methylpentanamido)methyl)-1H-imidazol-1-yl)methyl)-3'-fluoro-[1,1'-biphenyl]-2-carboxylic acid

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. R. Murray McKinnell, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med. Chem. Lett.

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